L21: Pharmacology Exam 1

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  1. Describe the 4 major eicosanoid receptors and their signaling pathways:
    • Relaxant: Gs - IP, EP2, EP4, DP1
    • Contractile: Gq, G12/13 (rho) and G16 - TP, FP, EP
    • Inhibitory: Gi - EP3
    • fMLP Receptor Family: Gi - DP2/CRH2
  2. What are the 3 major inflammatory functions of prostaglandins:
    • Pain: Hypealgesia by sensitizing neurons to bradykinin, histamine, 5-HT and substance P
    • Heat/Redness Production: PGE2 and PGI2
    • Swelling: Extravasation of fluid by other mediators
  3. Describe the effect of Prostacyclin (PGI2) on platelets? Where is it produced?
    • Produced by: Endothelium
    • Function: Inhibit aggregation, contribute to antithrombotic properties of endothelium and produce vasodilation
  4. What is the effect of Thromboxane (TXA2) on platelets? Where is it produced?
    • Prodyced by: Platelets
    • Function: Promote aggregation of platelets and produce vasoconstriction
  5. Describe the function of prostaglandins in the female reproductive system?
    • Non-Pregnant: PGF2 contracts uterus and causes CL regression, while PGE2 relaxes uterus
    • Pregnant: BOTH PGE2 and PGF2 contract uterus and PGF2 is important in parturition
    • In pregnancy, both levels continue to increase in amniotic fluid and blood
  6. Describe the functionof prostaglandins in the male reproductive tract? Where is it produced?
    • Produced in: Seminal vesicle, high amt found in semen
    • May help contraception by acting on cervix, uterine body, fallopian tubes
    • Low levels may correlate with infertility
  7. Describe the function of prostaglandins in the kidney?
    Function: Modulate blood flow, regulate urine and renin secretion
  8. Describe the SPECIAL function of PGE2 in the kidney
    • Vasodilate afferent arterioles
    • Lower sodium reabsorption
    • Increase renin scretion
  9. Describe the PG function in GI system? Which PG are especially important?
    • Function: Increase mucus secretion and water movement into lumen
    • PGE2 and PGI2: Inhibit vgastric acid secretion and produce vasodilation of gastric mucosa
  10. What PG are especially important in the pulmonary system? What is their function?
    • PGF2, PGD2 and TXA2: Contract bronchial smooth muscle
    • PGE1, PGE2, PGI2: Relax bronchial smooth muscle
  11. Describe function of PGE2 in CNS?
    • Increased in anterior HT by pyogens
    • Vasodilation in cerebral blood vessels (headache?)
  12. What prostaglandins are used in treatment of glaucoma?
    • Latanoprost
    • Bimatoprost
  13. What drugs are used in gastric/duodenal ulcer treatment?
    • Misoprost
    • Misoprost/Diclocfenac - with high NSAID use
  14. What drugs are used for early abortion induction?
    • Misoprostol
    • Carboprost
    • Dinoprostone
  15. What drugs are used for postpartum hemorrhage?
  16. What drugs are used for labor induction?
    • Dinoprostone
    • Carboprost
  17. What drugs are used to maintain the patency of DA?
  18. What drugs are used for ED?
  19. What drugs are used to treat pulmonary hypertension?
    • Epoprostanol
    • Iloprost
    • Treprostinii
  20. What conditions are treated using prostaglandins?
    • Glaucoma
    • Gastric/Duodenal Ulcers
    • Abortions (week 13-20)
    • Postpartum hemorrhage
    • Labor induction
    • Patency of ductus arteriosis
    • Erectile Dysfunction
    • Pulmonary hypertension
  21. Describe the effect of leukotrienes in the CV system - coronary and pulmonary arteries, endothelium permeability?
    • Coronary Artery: Constriction -  may be responsible for coronary artery vasospasms, cardiac anaphylaxis
    • Pulmonary Artery: Constriction
    • Endothelium: Increased permeability, exudation into tissue
    • Mediator of endotoxic shock
  22. What is a major function of LTB4 as pertaining to neutrophils, eosinophils and monocytes?
    • Promote PMN aggregation
    • Degranulation at higher concentrations
  23. What is the major funciton of LT in pulmonary system? Which one are important?
    • LTC4 and LTD4: Important in asthma and hypersensitivity
    • Made by mast cells
    • Vasoconstriction, mucus secretion, edema
  24. What is the major function of LT in renal system?
    • Vasoconstriction
    • Reduced GFR
    • May produce acute glomerular nephritis
  25. Describe mechanism, uses, S/E and special condsideration of Zafirlukast (Accolate)
    • Mechanism: LTD4 and LTE4 antagonist, inhibit bronchoconstriction
    • Use: Maintenance therapy for chronic asthma
    • S/E: Heaache, GI distrubance, pharyngitis, cough, rhinitis
    • Special: Metabolized by CYP2C9, weakly inhibits CYP3A4 and CYP2C9
    • Slow onset of action - caution in patients with liver disease
  26. Describe mechanism, uses, S/E and special condsideration of Montelukast (Singulair)
    • Mechanism: LTD4 receptor antagonist, inhibit bronchoconstriction
    • Use: Maintenace therapy for chronic asthma, exercise-induced asthma
    • S/E: Headache, cough, suicide, mood changes
    • Special: Metabolized by CYP3A4 and CYP2C9 but DOES NOT inhibit P450
    • Be careful of patients with aspirin-sensitive asthma
  27. Describe mechanism, uses, S/E and special condsideration of Zileuton (Zyflo)
    • Mechanism: 5-Lipoxygenase inhibitor, block ALL LT synthesis
    • Use: Maintenance therapy for chronic asthma
    • S/E: Dyspnea, flu-like symptoms, rare hepatitis
    • Special: Inhibits P450 system, monitor liver function
  28. What is the function of platelet activating factor in the pulmonary system?
    Longterm bronchoconstriction - may last 4 weeks
  29. What is the funciton of PAF in CV system?
    Hypotension independent of sympathetic tone
  30. What are some other functions of PAF?
    • Platelet aggregation
    • Leukocyte chemotaxis
    • IV-PAF resembles anaphylaxis
    • PAF generation = successful implantation and pregnancy
  31. What are potential pathophysiological functions of PAF?
    • Shock (hypotension)
    • Asthma (bronchoconstriction)
    • Inflammation - chemotaxis, degranulation, vasodilation
    • Anaphylaxis
    • Graph rejection
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L21: Pharmacology Exam 1
2012-09-08 18:15:44

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